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OBTAINING AND USING PHENYLCYCLOBUTYLAMIDE DERIVATIVES AND STEREOISOMERS THEREOF
专利权人:
BEJDZHING JANGU SENTURI FARMASI KO.; LTD
发明人:
ZhAO Shukjang (CN),ЖАО Шукянг (CN),VEN Shuming (CN),ВЕН Шуминг (CN),DING Khao (CN),ДИНГ Хао (CN),JaN Jashi (CN),ЯН Яши (CN),ChEN Ksjaoping (CN),ЧЕН Ксяопинг (CN),ZHAO SHUKJANG,ЖАО Шукянг,VEN SHUMING,ВЕН Шуминг,DING KHAO,ДИНГ Хао,JAN JASHI,ЯН Яши,CHEN KSJAOPING,ЧЕН Ксяопинг
申请号:
RU2010139017/04
公开号:
RU0002479572C2
申请日:
2009.03.24
申请国别(地区):
RU
年份:
2013
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to phenylcyclobutylamide derivatives of formula or a stereoisomer or pharmaceutically acceptable salt thereof. In formula (I), R is H, formacyl, acetyl, haloacetyl, benzoyl, benzyloxy carbonyl (Cbz), t-butoxy carbonyl (Boc), or 9-fluorenyl methoxyl carbonyl (Fmoc). The phenylcyclobutylamide derivative of formula (I), where R is H, is used to prepare medicine or a pharmaceutical composition for losing weight. The phenylcyclobutylamide derivatives of formula (I) are obtained by dissolving racemic or separate 1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutylamine and R-protected racemic or D- or L-isoleucine with anhydrous tetrahydrofuran; a condensing agent is then added in droplets to the solution which is then stirred at room temperature overnight, the precipitate is filtered and washed with anhydrous diethyl ether several times. The filtrate and anhydrous diethyl ether eluate are collected; a crude product is the obtained by evaporation, separation and pufification by column chromatography to obtain a racemic or optical isomeric compound, 2-(R-amino)-N-{1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl}-3-methylpentanamide; the R-protection group is removed to obtain a racemic or optical isomeric compound: 2-amino-N-{1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutyl}-3-methylpentanamide; a pharmaceutically acceptable acid is used to prepare a salt thereof.EFFECT: phenylcyclobutylamide derivatives which are suitable for treating obesity.7 cl, 1 tbl, 12 exИзобретение относится к производным фенилциклобутиламида формулы (I), его стереоизомеру или фармацевтически приемлемой соли. В формуле (I) R - это Н, формацил, ацетил, галоацетил, бензоил, бензилоксикарбонил (Cbz), t-бутоксикарбонил (Boc) или 9-флуоренилметоксилкарбонил (Fmoc). Производное фенилциклобутиламида формулы (I), где R - Н, используют для приготовления лекарства и фармацевтической композиции, предназначенных для снижения веса. Производные фенилциклобутиламида формулы
来源网站:
中国工程科技知识中心
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http://www.ckcest.cn/home/

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